Fujitani Y, Oda K, Takimoto M, Inui T, Okada T, Urade Y
International Research Laboratories, CIBA-GEIGY Limited, Takarazuka, Japan.
FEBS Lett. 1992 Feb 17;298(1):79-83. doi: 10.1016/0014-5793(92)80026-d.
Human umbilical vein endothelial cells (HUVECs) in primary culture produced and secreted endothelin 1 (ET-1) actively. Specific binding of [125I]ET-1 to these cells was not detectable because of the saturation of ET receptors with endogenously produced ET-1. However, addition of phosphoramidon, an inhibitor of ET-converting enzyme, to the medium reduced the production of ET-1 and thus the receptors on HUVECs were made available for exogenously added [125I]ET-1. Binding studies using phosphoramidon-treated HUVECs indicated the existence of a non-isopeptide-selective type (ETB) of ET receptor with a Kd of 17 pM. This receptor is thought to be involved in ET-induced vasodilation in an autocrine manner in vivo.
原代培养的人脐静脉内皮细胞（HUVECs）能活跃地产生并分泌内皮素1（ET-1）。由于内源性产生的ET-1使ET受体饱和，无法检测到[125I]ET-1与这些细胞的特异性结合。然而，向培养基中添加ET转换酶抑制剂磷酰胺素可减少ET-1的产生，从而使HUVECs上的受体可用于外源性添加的[125I]ET-1。使用经磷酰胺素处理的HUVECs进行的结合研究表明存在一种非异肽选择性类型（ETB）的ET受体，其解离常数（Kd）为17 pM。该受体被认为在体内以自分泌方式参与ET诱导的血管舒张。
